Pharmacological evaluation of Antidesma ghaesembilla Gaertn fruits for central nervous system depressant activity / Evaluación farmacológica de frutos de Antidesma ghaesembilla Gaertncomo depresores del sistema nervioso central

The objective of this study is to investigate the anxiolytic and sedative activities of the methanol and chloroform extracts of Antidesma ghaesembilla fruits at the dose of 400 mg/kg bw using rodent behavioral models such as thiopental sodium-induced sleeping time, hole cross method and open field process for sedative and its anxiolytic activity was evaluated using the elevated plus maze (EPM) methods. In case of thiopental sodium-induced sleeping time, both extracts exhibited dose dependent suppression of motor activity, exploratory behavior (in open field and hole cross method) and prolongation of thiopental sodium-induced sleeping time in mice, where maximum effect was shown by the methanol extract. In EPM test, the methanolic extract significantly increased exploration to and time spent by the treated mice in EPM open arms in a way similar to that of diazepam, but the chloroform extract was found to produce moderate activity. These significant results may justify the scientific basis for use of this plant in traditional medicine as a modality for anxiety and related disorders.

El objetivo de este estudio fue la investigación de las actividades ansiolíticas y sedantes de los extractos clorofórmicos y metabólicos de los frutos de Antidesma ghaesembilla a las dosis de 400 mg/kg pp utilizando modelos de comportamiento de roedores, tales como el tiempo de sueño inducido por tiopental sódico, el método de “hole cross” (cruce de un agujero) y el campo abierto para evaluar sedación, y la actividad ansiolítica fue evaluada utilizando el método del laberinto elevado (elevated plus maze, EPM). En el caso del sueño inducido por tiopental sódico, ambos extractos exhibieron una supresión dosis dependiente de la actividad motora, de la actividad exploratoria (en el método de campo abierto y “hole cross”) y prolongación del tiempo de inducción de sueño inducido por tiopental en ratones, con efectos máximos mostrados para el extracto metabólico. En el ensayo de EPM, el extracto metabólico aumentó significativamente el tiempo de exploración y el tiempo consumido en el laberinto de una manera similar al diazepam, pero el extracto clorofórmico se encontró que produjo solo una moderada actividad. Estos resultados significativos pueden justificar una base científica para el uso de plantas en medicina tradicional para tratar la ansiedad y desórdenes relacionados.

In vitro study on the interaction of ketotifen fumarate with anhydrous theophylline

The purpose of the present study was to investigate the interaction between ketotifen fumarate and anhydrous theophylline in aqueous media of various pH (1.2 and 6.8). Using Job's continuous-variation analysis and Ardon's spectrophotomeric measurement methods, the values of the stability constants of theophylline with ketotifen were determined at a fixed temperature (37 ºC) at various pH. The stability constants, ranging between 5.66 and 9.92, were derived from Ardon's plot, indicating that comparatively stable complexes had formed as a result of an interaction between the drugs. However, following the interaction of theophylline with ketotifen, stability constants were <1 at gastric pH (1.2) and intestinal pH (6.8). Concurrent administration of ketotifen and theophylline could result in the formation of a stable complex and this is likely to reduce the therapeutic activities of both drugs.

O objetivo do presente estudo foi investigar a interação entre o fumarato de cetotifeno e a teofilina anidra em meios aquosos com vários pH (1,2 e 6,8). Utilizando a análise da variação contínua de Job e os métodos de medida espectrofotométrica de Ardon, os valores das constantes de estabilidade da teofilina com o cetotifeno foram determinados em temperatura fixa (37 oC) em vários pH. As constantes de estabilidade, variando entre 5,66 e 9,92 derivaram-se a partir do delineamento de Ardon, indicando, comparativamente, que complexos estáveis se formaram como resultado da interação entre os fármacos. Entretanto, seguindo a interação da teofilina com o cetotifeno, as constantes de estabilidade foram <1, em pH gástrico (1,2) e intestinal (8,8). A administração concomitante de cetotifeno e teofilina poderia resultar na formação de complexo estável, o que reduz a atividade terapêutica de ambos os fármacos.